title: Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists.
abstract: High-throughput screening of the GSK compound collection against the P2Y(1) receptor identified a novel series of tetrahydro-4-quinolinamine antagonists. Optimal substitution around the piperidine group was pivotal for ensuring activity. An exemplar analog from this series was shown to inhibit platelet aggregation.
authors.affiliation: Department of Chemistry, Metabolic Pathways Centre for Excellence in Drug Discovery, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA 19406, USA. joseph.p.marino@gsk.com
authors.forename: Angel I
authors.initials: AI
authors.lastname: Morales-Ramos
authors.forename: John S
authors.initials: JS
authors.lastname: Mecom
authors.forename: Terry J
authors.initials: TJ
authors.lastname: Kiesow
authors.forename: Todd L
authors.initials: TL
authors.lastname: Graybill
authors.forename: Gregory D
authors.initials: GD
authors.lastname: Brown
authors.forename: Nambi V
authors.initials: NV
authors.lastname: Aiyar
authors.forename: Elizabeth A
authors.initials: EA
authors.lastname: Davenport
authors.forename: Lorena A
authors.initials: LA
authors.lastname: Kallal
authors.forename: Beth A
authors.initials: BA
authors.lastname: Knapp-Reed
authors.forename: Peng
authors.initials: P
authors.lastname: Li
authors.forename: Allyn T
authors.initials: AT
authors.lastname: Londregan
authors.forename: Dwight M
authors.initials: DM
authors.lastname: Morrow
authors.forename: Shobha
authors.initials: S
authors.lastname: Senadhi
authors.forename: Reema K
authors.initials: RK
authors.lastname: Thalji
authors.forename: Steve
authors.initials: S
authors.lastname: Zhao
authors.forename: Cynthia L
authors.initials: CL
authors.lastname: Burns-Kurtis
authors.forename: Joseph P
authors.initials: JP
authors.lastname: Marino
mesh_terms: D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D006801:Humans; D015394:Molecular Structure; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D058919:Purinergic P2 Receptor Antagonists; D018048:Receptors, Purinergic P2 / Q000378:metabolism; D058472:Receptors, Purinergic P2Y1; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013927:Thrombosis / Q000188:drug therapy
chemical_list: C534104:1,2,3,4-tetrahydro-4-quinolinamine; D000634:Aminoquinolines; C546382:P2RY1 protein, human; D010975:Platelet Aggregation Inhibitors; D058919:Purinergic P2 Receptor Antagonists; D018048:Receptors, Purinergic P2; D058472:Receptors, Purinergic P2Y1